Literature DB >> 20594842

Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties.

Tara R Rheault1, Kelly H Donaldson, Jennifer G Badiang-Alberti, Ronda G Davis-Ward, C Webb Andrews, Ramesh Bambal, Jeffrey R Jackson, Mui Cheung.   

Abstract

Potent inhibitors of PLK1 with acceptable solubility, mouse iv clearance, and reduced CYP450 inhibition were identified. Drug-like properties were improved using a heteroaryl ring as a functional handle for manipulation of inhibitors' physiochemical and DMPK properties. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20594842     DOI： 10.1016/j.bmcl.2010.06.009

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  4 in total

1.  Host cell and expression engineering for development of an E. coli ketoreductase catalyst: enhancement of formate dehydrogenase activity for regeneration of NADH.

Authors:  Katharina Mädje; Katharina Schmölzer; Bernd Nidetzky; Regina Kratzer
Journal:  Microb Cell Fact       Date:  2012-01-11       Impact factor: 5.328

2.  Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (PLK1), a Potential Drug Target in Schistosoma mansoni.

Authors:  Thavy Long; R Jeffrey Neitz; Rachel Beasley; Chakrapani Kalyanaraman; Brian M Suzuki; Matthew P Jacobson; Colette Dissous; James H McKerrow; David H Drewry; William J Zuercher; Rahul Singh; Conor R Caffrey
Journal:  PLoS Negl Trop Dis       Date:  2016-01-11

3.  Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.

Authors:  Laura A T Cleghorn; Peter C Ray; Joshua Odingo; Anuradha Kumar; Heather Wescott; Aaron Korkegian; Thierry Masquelin; Abraham Lopez Moure; Caroline Wilson; Susan Davis; Margaret Huggett; Penelope Turner; Alasdair Smith; Ola Epemolu; Fabio Zuccotto; Jennifer Riley; Paul Scullion; Yoko Shishikura; Liam Ferguson; Joaquin Rullas; Laura Guijarro; Kevin D Read; Simon R Green; Phil Hipskind; Tanya Parish; Paul G Wyatt
Journal:  J Med Chem       Date:  2018-07-26       Impact factor: 7.446

4.  Bioluminescent Zebrafish Transplantation Model for Drug Discovery.

Authors:  Martina Hason; Jovana Jovicic; Ivana Vonkova; Milan Bojic; Theresa Simon-Vermot; Richard M White; Petr Bartunek
Journal:  Front Pharmacol       Date:  2022-04-27       Impact factor: 5.988
  4 in total

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